Fmoc-Val-Cit-PAB-PNP

Research use only, not for human use.

A cathepsin B-cleavable dipeptide linker for antibody-drug-conjugation (ADC).

A cathepsin B-cleavable dipeptide linker for antibody-drug-conjugation (ADC).

Fmoc-Val-Cit-PAB-PNP contains peptide sequence degradable by a lysosome enzyme.Cathepsin B in the lysosome cleaves the peptide bond between Cit-PAB of dipeptide linkers containing Valine (Val)-citrulline (Cit) and p-aminobenzylalcohol (PAB). When PAB and a drug are binded covalently with carbamate bonds, the drug can be released by hydrolysis after cleavage of the peptide bond between Cit-PAB. Antibody-drug conjugates (ADCs) has been developed using this mechanism.

Fmoc-Val-Cit-PAB-PNP linker stabilization in the mouse is an essential prerequisite for designing successful efficacy and safety studies in rodents during preclinical stages of ADC programs. Conjugation site plays an important role in determining VC-PABC linker stability in mouse plasma, and that the stability of the linker positively correlates with ADC cytotoxic potency both in vitro and in vivo.

Fmoc-Val-Cit-PAB-PNP

Antibody Drug Conjugates (ADC)

ADCs Linker/Click Chemistry

ADCs Linker/Click Chemistry

Other Indications

——

863971-53-3

766.7957

C40H42N6O10

>98% (HPLC)

DMSO: ≥ 40 mg/mL

O=C(OCC1=CC=C(NC([C@H](CCCNC(N)=O)NC([C@H](C(C)C)NC(OCC2C(C=CC=C3)=C3C4=C2C=CC=C4)=O)=O)=O)C=C1)OC5=CC=C([N+]([O-])=O)C=C5

L-Ornithinamide, N-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-valyl-N5-(aminocarbonyl)-N-[4-[[[(4-nitrophenoxy)carbonyl]oxy]methyl]phenyl]-

(-20℃)

With Ice Pack

≥ 2 years